Jump to main content
Jump to site search

Issue 24, 2018
Previous Article Next Article

Methylene-linked bis-phenylbenzimidazoles – a new scaffold to target telomeric DNA/RNA hybrid duplex

Author affiliations

Abstract

We report a series of novel methylene-linked bis-phenylbenzimidazoles intercalators that stabilize telomeric DNA/RNA hybrid (tDRH) structures by up to 7.2 °C at a 1 μM ligand concentration while having negligible affinity for DNA/DNA duplexes, although with a low affinity for quadruplex DNA. We have used molecular modelling studies to rationalize this selectivity, concluding that the methylene spacer between the terminal benzimidazole and phenylene moieties plays a key role in facilitating the bis-intercalating process. This scaffold may be used to develop chemical tools or new therapeutics to selectively target the telomeric DNA/RNA duplex without affecting normal genomic DNA.

Graphical abstract: Methylene-linked bis-phenylbenzimidazoles – a new scaffold to target telomeric DNA/RNA hybrid duplex

Back to tab navigation

Supplementary files

Publication details

The article was received on 03 Nov 2017, accepted on 12 Jan 2018 and first published on 02 Mar 2018


Article type: Communication
DOI: 10.1039/C7OB02709E
Citation: Org. Biomol. Chem., 2018,16, 4424-4428
  •   Request permissions

    Methylene-linked bis-phenylbenzimidazoles – a new scaffold to target telomeric DNA/RNA hybrid duplex

    M. K. Islam, P. J. M. Jackson, D. E. Thurston and K. M. Rahman, Org. Biomol. Chem., 2018, 16, 4424
    DOI: 10.1039/C7OB02709E

Search articles by author

Spotlight

Advertisements